Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors

Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors

A total of Twenty two (22) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1HNMR, 13C NMR and screened against cholinesterase inhibitory potentials. All the adducts (1–22) showed varying degree of cholinesterase inhibitory potential IC50 ranging between...

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Published in:Chemical Data Collections
Main Author: Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
Format: Data paper
Language:English
Published: Elsevier B.V. 2024
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85196391388&doi=10.1016%2fj.cdc.2024.101151&partnerID=40&md5=0bd0bb78f06662cc2b9bdd453c330d2f
id 2-s2.0-85196391388
spelling 2-s2.0-85196391388
Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
2024
Chemical Data Collections
52

10.1016/j.cdc.2024.101151
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85196391388&doi=10.1016%2fj.cdc.2024.101151&partnerID=40&md5=0bd0bb78f06662cc2b9bdd453c330d2f
A total of Twenty two (22) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1HNMR, 13C NMR and screened against cholinesterase inhibitory potentials. All the adducts (1–22) showed varying degree of cholinesterase inhibitory potential IC50 ranging between 13.23 ± 0.02 to 59.09 ± 1.22 µM against acetylcholinesterase, with IC50 values ranging from 23.55 ± 0.32 to 61.55 ± 0.58 µM against butyrylcholinesterase. Among the series analogs 1, 3, 8, 12, 14, 15, 17, 18 and 22 with IC50 values 20.05 ± 0.13, 17.32 ± 0.15, 14.32 ± 0.97, 23.33 ± 0.56, 18.02 ± 0.09, 19.05 ± 0.13, 15.11 ± 0.23, 13.23 ± 0.02, and 22.57 ± 0.09 µM respectively showed excellent inhibitory potential against acetylcholinesterase and with IC50 values 31.46 ± 0.98, 26.06 ± 0.08, 25.33 ± 1.49, 30.12 ± 0.78, 28.11 ± 0.5, 29.33 ± 0.19, 25.37 ± 0.47, 23.55 ± 0.32 and 33.12 ± 0.78 against butylcholinesterase as compared to the standard Galanthamine. All other analogs showed moderate inhibitory potential. A structure-activity relationship has been established for all compounds. Through molecular docking studies, the interactions between compounds with the enzyme active sites were confirmed. © 2024
Elsevier B.V.
24058300
English
Data paper
author Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
spellingShingle Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
author_facet Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
author_sort Zulfiqar A.; Khan I.U.; Nabi M.; Ullah H.; Iqbal N.; Zeb B.; Hussain A.; Khan D.; Rab A.; Junaid S.M.; Taha M.; Shah S.A.A.; Rahim F.
title Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
title_short Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
title_full Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
title_fullStr Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
title_full_unstemmed Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
title_sort Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
publishDate 2024
container_title Chemical Data Collections
container_volume 52
container_issue
doi_str_mv 10.1016/j.cdc.2024.101151
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85196391388&doi=10.1016%2fj.cdc.2024.101151&partnerID=40&md5=0bd0bb78f06662cc2b9bdd453c330d2f
description A total of Twenty two (22) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1HNMR, 13C NMR and screened against cholinesterase inhibitory potentials. All the adducts (1–22) showed varying degree of cholinesterase inhibitory potential IC50 ranging between 13.23 ± 0.02 to 59.09 ± 1.22 µM against acetylcholinesterase, with IC50 values ranging from 23.55 ± 0.32 to 61.55 ± 0.58 µM against butyrylcholinesterase. Among the series analogs 1, 3, 8, 12, 14, 15, 17, 18 and 22 with IC50 values 20.05 ± 0.13, 17.32 ± 0.15, 14.32 ± 0.97, 23.33 ± 0.56, 18.02 ± 0.09, 19.05 ± 0.13, 15.11 ± 0.23, 13.23 ± 0.02, and 22.57 ± 0.09 µM respectively showed excellent inhibitory potential against acetylcholinesterase and with IC50 values 31.46 ± 0.98, 26.06 ± 0.08, 25.33 ± 1.49, 30.12 ± 0.78, 28.11 ± 0.5, 29.33 ± 0.19, 25.37 ± 0.47, 23.55 ± 0.32 and 33.12 ± 0.78 against butylcholinesterase as compared to the standard Galanthamine. All other analogs showed moderate inhibitory potential. A structure-activity relationship has been established for all compounds. Through molecular docking studies, the interactions between compounds with the enzyme active sites were confirmed. © 2024
publisher Elsevier B.V.
issn 24058300
language English
format Data paper
accesstype
record_format scopus
collection Scopus
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